评估将茶夫(Eragrostis tef)谷物中的抗性淀粉作为结肠靶向给药薄膜包衣材料的效果

bioRxiv Pub Date : 2024-08-08 DOI:10.1101/2024.08.06.606940
Yohannes Teshome, A. Belete, T. Gebre-Mariam
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引用次数: 0

摘要

特夫(Eragrostis tef,菊科)是埃塞俄比亚广泛种植的一种原生谷类作物,含有约 73% 的碳水化合物,其中约 30% 为抗性淀粉。本研究评估了从teff谷物中提取的抗性淀粉作为一种薄膜包衣材料,用于结肠靶向给药甲硝唑(用作模型药物)。从茶叶中提取淀粉,并从总淀粉中分离出抗性淀粉。采用湿法制粒法制备了甲硝唑芯片,压制后涂覆了抗性淀粉薄膜。片剂的理化特性在体外进行了评估。为防止抗性淀粉的主要成分直链淀粉膨胀导致薄膜过早破坏,添加了一种水不溶性聚合物乙基纤维素。我们使用了不同比例的直链淀粉和乙基纤维素作为薄膜包衣材料,并在模拟条件下进行了评估,以确定在结肠(而非上消化道)释放药物的最佳组合。溶解和发酵研究的结果表明,淀粉糖与乙基纤维素的最佳薄膜包衣比例以及相应厚度占总增重的百分比为厚度为 6% 时为 1:1,厚度为 4% 和 6% 时为 1:2,厚度为 2% 和 4% 时为 1:3。薄膜材料的定向药物释放归功于结肠中细菌酶对抗性淀粉成分的消化。抗性淀粉被消化后会在乙基纤维素薄膜支架上形成孔隙,从而导致薄膜破裂,药物完全在细菌微生物群居住的结肠中释放出来。基于这些结果,茶夫谷物中的抗性淀粉显示出作为结肠靶向辅料的潜力。
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Evaluation of resistant starch from teff (Eragrostis tef) grain as a film coating material for colon-targeted drug delivery
Teff (Eragrostis tef, family Poaceae) is a native cereal crop widely grown in Ethiopia, containing approximately 73% carbohydrates, of which about 30% is resistant starch. This study evaluates resistant starch extracted from teff grain as a film coating material for colon-targeted delivery of metronidazole, used as a model drug. Starch was extracted from teff and resistant starch was isolated from the total starch. Metronidazole core tablets were prepared by wet granulation, compressed, and coated with a resistant starch-based film. The physicochemical properties of the tablets were evaluated in vitro. To prevent premature film disruption caused by the swelling of amylose, a dominant component of resistant starch, a water-insoluble polymer, ethylcellulose, was added. Various proportions of amylose and ethylcellulose were used as film coating materials and evaluated in simulated conditions to determine the optimal combination for drug release in the colon, but not in the upper gastrointestinal tract. The results of the dissolution and fermentation studies indicated the best film coating proportions of amylose to ethylcellulose and the corresponding thicknesses in percentage of total weight gain were: 1:1 ratio at 6% thickness, 1:2 ratio at 4% and 6% thickness, and 1:3 ratio at 2% and 4% thickness. The targeted drug release of the film material is attributed to bacterial enzyme digestion of the resistant starch component in the colon. The digestion of resistant starch creates pores in the ethylcellulose film scaffold, leading to the disruption of the film and release of the drug exclusively in the colon, where the bacterial microflora reside. Based on these results, resistant starch from teff grain shows potential as a colon-targeting excipient.
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